Delivery of proteins across polar epithelial cell layers

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01)

Patent

CA 2389302

This invention provides bioactive conjugates. The bioactive conjugates include: (1) a cell recognition moiety that binds to .alpha.2 macroglobulin receptor .alpha.2-MR and (2) a bioactive moiety which: (a) has a biological activity, (b) does not function solely as an immunogen to invoke an immune response and (c) does not have ADP ribosylating activity. The bioactive conjugates of this invention are useful in methods of transporting the bioactive moiety across a polar epithelial membrane. Thus, this invention provides methods for parenteral administration of proteins without injection.

La présente invention concerne des conjugués bioactifs comprenant : (1) un fragment de reconnaissance cellulaire qui se lie à un récepteur de macroglobuline .alpha.¿2? (.alpha.2-MR) et (2) un fragment bioactif qui (a) présente une activité biologique, (b) ne fonctionne pas uniquement en tant qu'immunogène pour induire une réponse immunitaire et (c) ne présente pas d'activité d'ADP-ribosylation. Les conjugués bioactifs selon cette invention sont utilisés dans des procédés de transport du fragment bioactif à travers une membrane épithéliale polaire. Ainsi, cette invention concerne des procédés d'administration parentérale de protéines, sans injection.

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